公开(公告)号：US20180258062A1

公开(公告)日：2018-09-13

申请号：US15974494

申请日：2018-05-08

申请人： UBE INDUSTRIES, LTD.

发明人： Noriaki IWASE ,  Hiroshi NISHIDA ,  Makoto OKUDO ,  Masaaki ITO ,  Shigeyuki KONO ,  Masaaki MATOYAMA ,  Shigeru USHIYAMA ,  Eiji OKANARI ,  Hirofumi MATSUNAGA ,  Kenji NISHIKAWA ,  Tomio KIMURA

IPC分类号： C07D333/36 ,  A61K31/443 ,  A61K31/427 ,  A61K31/381 ,  C07D417/12 ,  C07D409/14 ,  C07D409/04 ,  C07D409/12

摘要： A novel α-halogen-substituted thiophene compound or a pharmacologically acceptable salt thereof, which has a potent LPA receptor-antagonist activity and is useful as a medicament is provided. A compound represented by the general formula (I) wherein A represents, a phenyl ring, a thiophene ring, or an isothiazole ring; R1 is the same or different, and represents a halogen atom, or a C1-C3 alkyl group; R2 represents a hydrogen atom, or a C1-C6 alkyl group; p represents an integer of 0 to 5; V represents CR3 wherein R3 represents a hydrogen atom, an amino group, a nitro group, or a C1-C3 alkoxy group, or V represents a nitrogen atom; and X represents a halogen atom, or a salt thereof.

公开(公告)号：US20190256531A1

公开(公告)日：2019-08-22

申请号：US16373840

申请日：2019-04-03

申请人： UBE INDUSTRIES, LTD.

发明人： Noriaki IWASE ,  Yasuhiro AGA ,  Shigeru USHIYAMA ,  Shigeyuki KONO ,  Hidetoshi SUNAMOTO ,  Takashi MATSUSHITA ,  Sayaka OGI ,  Satoshi UMEZAKI ,  Masahiro KOJIMA ,  Kazuhiro ONUMA ,  Yusuke SHIRAISHI ,  Makoto OKUDO ,  Tomio KIMURA

IPC分类号： C07F7/08 ,  A61K45/06 ,  A61P35/00 ,  A61K31/695 ,  C07F7/10 ,  C07F7/12

摘要： The present invention provides a compound represented by the general formula (Ia) or a pharmacologically acceptable salt thereof. In the general formula (Ia), two R moieties each independently represent a C1-3 alkyl group or the like; and R1, R2 and R3 each independently represent an optionally substituted linear or branched C1-4 alkyl group.

公开(公告)号：US20170313727A1

公开(公告)日：2017-11-02

申请号：US15522592

申请日：2015-10-30

申请人： UBE INDUSTRIES, LTD.

发明人： Yasuhiro AGA ,  Shigeru USHIYAMA ,  Noriaki IWASE ,  Shigeyuki KONO ,  Hidetoshi SUNAMOTO ,  Takashi MATSUSHITA ,  Sayaka OGI ,  Masayuki TANAKA ,  Masaaki MATOYAMA ,  Satoshi UMEZAKI ,  Yusuke SHIRAISHI ,  Kazuhiro ONUMA ,  Masahiro KOJIMA ,  Hayato NISHIYAMA ,  Tomio KIMURA

IPC分类号： C07F7/10

CPC分类号： C07F7/10 ,  A61K31/695 ,  Y02P20/55

摘要： Provided is a compound represented by formula (I) or a pharmacologically acceptable salt thereof: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.

公开(公告)号：US20150376160A1

公开(公告)日：2015-12-31

申请号：US14752623

申请日：2015-06-26

申请人： UBE INDUSTRIES, LTD.

发明人： Noriaki IWASE ,  Hiroshi NISHIDA ,  Makoto OKUDO ,  Masaaki ITO ,  Shigeyuki KONO ,  Masaaki MATOYAMA ,  Shigeru USHIYAMA ,  Eiji OKANARI ,  Hirofumi MATSUNAGA ,  Kenji NISHIKAWA ,  Tomio KIMURA

IPC分类号： C07D333/36 ,  C07D409/14 ,  C07D417/12 ,  C07D409/04 ,  C07D409/12

CPC分类号： C07D333/36 ,  A61K31/381 ,  A61K31/427 ,  A61K31/443 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

摘要： A novel α-halogen-substituted thiophene compound or a pharmacologically acceptable salt thereof, which has a potent LPA receptor-antagonist activity and is useful as a medicament is provided.A compound represented by the general formula (I) wherein A represents, a phenyl ring, a thiophene ring, or an isothiazole ring; R1 is the same or different, and represents a halogen atom, or a C1-C3 alkyl group; R2 represents a hydrogen atom, or a C1-C6 alkyl group; p represents an integer of 0 to 5; V represents CR3 wherein R3 represents a hydrogen atom, an amino group, a nitro group, or a C1-C3 alkoxy group, or V represents a nitrogen atom; and X represents a halogen atom, or a salt thereof.

摘要翻译： 提供了一种具有强效LPA受体 - 拮抗剂活性并可用作药物的新型α-卤素取代噻吩化合物或其药理学上可接受的盐。 由通式（I）表示的化合物，其中A表示苯基环，噻吩环或异噻唑环; R1相同或不同，表示卤素原子或C1-C3烷基; R2表示氢原子或C1-C6烷基; p表示0〜5的整数， V表示CR 3，其中R3表示氢原子，氨基，硝基或C1-C3烷氧基，或V表示氮原子; X表示卤素原子或其盐。

公开(公告)号：US20190062353A1

公开(公告)日：2019-02-28

申请号：US16174704

申请日：2018-10-30

申请人： UBE INDUSTRIES, LTD.

发明人： Noriaki IWASE ,  Shigeyuki KONO ,  Masayuki TANAKA ,  Masaaki MATOYAMA ,  Satoshi UMEZAKI ,  Yusuke SHIRAISHI ,  Masahiro KOJIMA ,  Hayato NISHIYAMA

IPC分类号： C07F7/10 ,  A61K31/695

摘要： Methods of producing a compound represented by formula (I) or a pharmacologically acceptable salt thereof include: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.

公开(公告)号：US20180186818A1

公开(公告)日：2018-07-05

申请号：US15736677

申请日：2016-06-14

申请人： UBE INDUSTRIES, LTD.

发明人： Noriaki IWASE ,  Yasuhiro AGA ,  Shigeru USHIYAMA ,  Shigeyuki KONO ,  Hidetoshi SUNAMOTO ,  Takashi MATSUSHITA ,  Sayaka OGI ,  Satoshi UMEZAKI ,  Masahiro KOJIMA ,  Kazuhiro ONUMA ,  Yusuke SHIRAISHI ,  Makoto OKUDO ,  Tomio KIMURA

IPC分类号： C07F7/08 ,  A61P35/00 ,  A61K31/695 ,  A61K45/06

CPC分类号： C07F7/0812 ,  A61K31/695 ,  A61K45/06 ,  A61P35/00 ,  C07F7/10 ,  C07F7/12

摘要： The present invention provides a compound represented by the general formula (Ia) or a pharmacologically acceptable salt thereof. In the general formula (Ia), two R moieties each independently represent a C1-3 alkyl group or the like; and R1, R2 and R3 each independently represent an optionally substituted linear or branched C1-4 alkyl group.

公开(公告)号：US20170158663A1

公开(公告)日：2017-06-08

申请号：US15321633

申请日：2015-06-26

申请人： UBE INDUSTRIES, LTD.

发明人： Noriaki IWASE ,  Hiroshi NISHIDA ,  Makoto OKUDO ,  Masaaki ITO ,  Shigeyuki KONO ,  Masaaki MATOYAMA ,  Shigeru USHIYAMA ,  Eiji OKANARI ,  Hirofumi MATSUNAGA ,  Kenji NISHIKAWA ,  Tomio KIMURA

IPC分类号： C07D333/36

CPC分类号： C07D333/36 ,  A61K31/381

摘要： The invention provides a novel α-halogen-substituted thiophene compound salt that has a potent LPA receptor antagonistic action and is useful as a medicament. The salt is represented by the general formula (I): (wherein R is a hydrogen atom or a methoxy group; X is a halogen atom; A is selected from the group consisting of: ;M is an alkali metal or an alkaline earth metal; and n is 1 when M is an alkali metal and is 2 when M is an alkaline earth metal).